Composition and method for inhibition of nerve transmission

a technology of nerve transmission and composition, which is applied in the direction of biocide, plant/algae/fungi/lichens ingredients, drug compositions, etc., can solve the problems of limiting the use of populations, amitriptyline has a high incidence of anticholinergic side effects, and the success of neuropathic pain treatment with these approaches is limited. , to achieve the effect of inhibiting nerve cell transmission

Active Publication Date: 2011-10-20
NEUROQUEST INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0031]and, optionally, one or more pharmaceutically acceptable diluent or excipient.
[0032]In accordance with another aspect of the presently claimed and disclosed invention(s), there is provided a method of treating a disorder characterized by an imbalance between nerve excitation and inhibition comprising administering a therapeutically effective amount of a composition as described herein to a mammalian subject, wherein said therapeutically effective amount is an amount that inhibits nerve cell transmission. The mammalian subject is preferably a human. Preferably, the method of the presently claimed and disclosed invention(s) is for the treatment of neuropathic pain, which can be caused by, for example, diabetic peripheral neuropathy, herpes zoster, post herpetic neuralgia, trigeminal neuralgia, complex regional pain syndrome, reflex sympathetic dystrophy, phantom limb syndrome, chronic disease (multiple sclerosis, HIV, etc), trauma (c

Problems solved by technology

Nociceptive pain usually responds to opioids and non-steroidal anti-inflammatories (NSAIDS), whereas the success of treating neuropathic pain with these approaches has been limited.
Amitriptyline has a high incidence of anticholinergic side effects, including delirium in elderly patients.
TCAs also have proarrhythmic effects which limit their use in populations with abnormal EKG.
However, ketamine causes sedation, slowed reaction times and hallucinations with long-term use.
It has been used with some success to decrease pain in patients with diabetic neuropathy, but has not benefited those with postherpetic neuralgia, post stroke pain, or peripheral neuropathies other than diabetic.
It may act on unmyelinated primary afferent nerves by depleting substance P. Depletion requires repeated and consistent use of capsaicin, and patient compliance can be an issue due to the common side effect of an intense burning sensation that decreases with consistent use.
Overall, relief with capsaicin cream in clinical trials of neuropathic pain has been inconsistent.
Overall, the efficacy of th

Method used

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  • Composition and method for inhibition of nerve transmission
  • Composition and method for inhibition of nerve transmission
  • Composition and method for inhibition of nerve transmission

Examples

Experimental program
Comparison scheme
Effect test

example 1

Patch Clamp Electrophysiological recordings (K+ Channels

[0098]Potassium channels have been associated with a number of important cellular functions including the regulation of heart rate, muscle contraction, neurotransmitter release, and neuronal excitability (14). As such, K+ channels have been recognized as potential drug targets and have been utilized as screening agents for potential therapeutic molecules, including potential therapeutic drugs for pain. The role of K+ channels in controlling cell membrane potential and neuronal cellular excitability makes them of interest in modulating neruronal hyperexcitability states, including neuropathic pain.

[0099]Whole cell patch clamp recordings (Axopatch 200B) were made using borosilicate patch pipettes of resistance 3-8 MΩ with an intracellular solution utilizing potassium chloride as the current carrier. Current clamp recording were conducted holding the membrane potential at −60 mV to characterize the firing property of the cells. Vo...

example 2

Human Screening Using Synthetic Geranium in Neuropathic Pain (Post-Herpetic Neuralgia)

[0101]Since natural geranium oil relieves neuropathic pain and inhibits the delayed rectifying potassium channel, and since synthetic geranium oil, geraniol, and citronellol all inhibit the delayed rectifying potassium channel, synthetic geranium oil and geraniol were tested on patients with post-herpetic neuralgia. A synthetic blend of geranium oil was tested in patients with post-herpetic neuralgia that were positive responders to natural geranium oil. Pain relief with a synthetic blend of geranium oil (see Table 1 for constituents their relative amounts in the synthetic blend) was self reported to be as good or better than pain relief with natural geranium oil. Pure geraniol was then tested in these subjects. Results indicated that geraniol had the greatest effect on neuropathic pain relief.

example 3

Human Clinical Trial of 64 Patients with all Cause Neuropathy

[0102]A total of 64 individuals with diagnosed peripheral neuropathy of at least 3 months duration and experiencing daily plantar cutaneous foot pain were recruited and screened for eligibility. Of these individuals, 18 were excluded because they did not meet the predetermined inclusion criteria for foot pain (VAS=3-8). The remaining participants completed three weeks of pain-relieving intervention as described below. One participant did not complete the intervention due to unknown reasons. Of those participants that competed all testing procedures (n=45), five participants reported pre-test foot pain levels outside of the predetermined criteria (VAS 8) at least once throughout the study period. All data acquired from these participants was excluded from subsequent analyses. There was no adverse event during the study period to report.

[0103]Pain was recorded before treatment and for 8 hrs after treatment on an 11 point (0-...

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Abstract

The presently claimed and disclosed invention(s) provides a therapeutically effective composition and method of inhibiting nerve cell transmission. In a preferred embodiment of the presently claimed and disclosed invention(s), the treatment of neuropathic pain utilizing terpene compounds isolated from plant essential oils or manufactured synthetically is detailed. These compounds, such as geraniol and citronellol, as well as chemical analogs thereof, used in combination or individually, can be used alone or in a composition with a pharmaceutically acceptable carrier in a suitable dosage form.

Description

CROSS REFERENCE TO RELATED APPLICATION[0001]This application claims the benefit and priority to co-pending PCT / CA2008 / 000236, having an international filing date of Feb. 6, 2008, which claims benefit and priority to U.S. provisional patent application No. 60 / 899,642, filed Feb. 6, 2007, which is incorporated herein in its entirety as though set forth explicitly herein.FIELD OF THE INVENTION[0002]The presently claimed and disclosed invention(s) pertains to the field of compositions comprising one or more aromatic terpene compound. More specifically, the presently claimed and disclosed invention(s) pertains to non-naturally occurring compositions comprising an aromatic terpene compound, and methods of using such compositions for the inhibition of nerve cell transmission.BACKGROUND[0003]Ideal physiological functioning requires an appropriate balance between nerve cell excitation and inhibition. Therefore, the identification of compounds, and methods of utilizing these compounds, to alt...

Claims

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Application Information

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IPC IPC(8): A61K31/045A61P25/00A61K31/22A61K31/122A61K31/351A61K31/11
CPCA61K31/045A61K31/121A61K31/351A61K31/22A61K31/122A61K31/11A61K2300/00A61P25/00A61P25/02A61P25/04A61P29/00A61K36/185
Inventor MCLELLAN, ALEXANDERGREENWAY, FRANK
Owner NEUROQUEST INC
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